Literature DB >> 20137939

Design, synthesis and biological evaluation of estradiol-chlorambucil hybrids as anticancer agents.

Atul Gupta1, Pijus Saha, Caroline Descôteaux, Valérie Leblanc, Eric Asselin, Gervais Bérubé.   

Abstract

A series of estradiol-chlorambucil hybrids was synthesized as anticancer drugs for site-directed chemotherapy of breast cancer. The novel compounds were synthesized in good yields through efficient modifications of estrone at position 16alpha of the steroid nucleus. The newly synthesized compounds were evaluated for their anticancer efficacy in different hormone-dependent and hormone-independent breast cancer cell lines. The novel hybrids showed significant in vitro anticancer activity when compared to chlorambucil. Structure-activity relationship (SAR) reveals the influence of the length of the spacer chain between carrier and drug molecule. Copyright 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 20137939     DOI： 10.1016/j.bmcl.2010.01.053

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  6 in total

1.  Design, synthesis, and initial biological evaluation of a steroidal anti-estrogen-doxorubicin bioconjugate for targeting estrogen receptor-positive breast cancer cells.

Authors:  Kinh-Luan Dao; Rupa R Sawant; J Adam Hendricks; Victoria Ronga; Vladimir P Torchilin; Robert N Hanson
Journal:  Bioconjug Chem       Date:  2012-04-04       Impact factor: 4.774

Review 2.  Multimarker screening of oxidative stress in aging.

Authors:  Kamila Syslová; Adéla Böhmová; Miloš Mikoška; Marek Kuzma; Daniela Pelclová; Petr Kačer
Journal:  Oxid Med Cell Longev       Date:  2014-07-16       Impact factor: 6.543

3.  Metasequoia glyptostroboides potentiates anticancer effect against cervical cancer via intrinsic apoptosis pathway.

Authors:  Hoomin Lee; Cheolwoo Oh; Suji Kim; Debasish Kumar Dey; Hyung Kyo Kim; Vivek K Bajpai; Young-Kyu Han; Yun Suk Huh
Journal:  Sci Rep       Date:  2021-01-13       Impact factor: 4.379

4.  Promising Hybrids Derived from S-Allylcysteine and NSAIDs Fragments against Colorectal Cancer: Synthesis, In-vitro Evaluation, Drug-Likeness and In-silico ADME/tox Studies.

Authors:  Angie Herrera-R; Wilson Castrillón; Manuel Pastrana; Andres F Yepes; Wilson Cardona-G
Journal:  Iran J Pharm Res       Date:  2021       Impact factor: 1.696

5.  New Hybrids Based on Curcumin and Resveratrol: Synthesis, Cytotoxicity and Antiproliferative Activity against Colorectal Cancer Cells.

Authors:  Cristian Hernández; Gustavo Moreno; Angie Herrera-R; Wilson Cardona-G
Journal:  Molecules       Date:  2021-05-01       Impact factor: 4.411

6.  Synthesis and in-vitro Evaluation of S-allyl Cysteine Ester - Caffeic Acid Amide Hybrids as Potential Anticancer Agents.

Authors:  Wilson Castrillón; Angie Herrera-R; Laura Juliana Prieto; Laura Conesa-Milián; Miguel Carda; Tonny Naranjo; Maria Elena Maldonado; Wilson Cardona-G
Journal:  Iran J Pharm Res       Date:  2019       Impact factor: 1.696
  6 in total

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